BRPI0515935B8 - pirimidinas heterociclil- ou 5-carbo substituídas para inibição de hiv, e composição farmacêutica - Google Patents

pirimidinas heterociclil- ou 5-carbo substituídas para inibição de hiv, e composição farmacêutica

Info

Publication number
BRPI0515935B8
BRPI0515935B8 BRPI0515935A BRPI0515935A BRPI0515935B8 BR PI0515935 B8 BRPI0515935 B8 BR PI0515935B8 BR PI0515935 A BRPI0515935 A BR PI0515935A BR PI0515935 A BRPI0515935 A BR PI0515935A BR PI0515935 B8 BRPI0515935 B8 BR PI0515935B8
Authority
BR
Brazil
Prior art keywords
alkyl
optionally substituted
substituted
amino
alkyloxy
Prior art date
Application number
BRPI0515935A
Other languages
English (en)
Inventor
Heeres Jan
Emile Georges Guillemont Jérôme
Joannes Lewi Paulus
Original Assignee
Janssen Sciences Ireland Uc
Janssen R&D Ireland
Tibotec Pharm Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Janssen Sciences Ireland Uc, Janssen R&D Ireland, Tibotec Pharm Ltd filed Critical Janssen Sciences Ireland Uc
Publication of BRPI0515935A publication Critical patent/BRPI0515935A/pt
Publication of BRPI0515935B1 publication Critical patent/BRPI0515935B1/pt
Publication of BRPI0515935B8 publication Critical patent/BRPI0515935B8/pt

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/50—Three nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

pirimidinas heterociclil- ou 5-carbo substituídas para inibição de hiv. inibidores de replicação de hiv da fórmula (i), n-óxidos, sais de adição farmaceuticamente aceitáveis, aminas quaternárias ou formas estereoisoméricas dos mesmos, em que: - a1 = a2 - a3 = a4 é -ch=ch=ch=ch-, -n=ch-ch=ch, -n=ch-n=ch-, -n=ch-ch=n, -n=n-ch=ch; -b1 = b2 - b3 = b4 é -ch=ch-ch=ch, -n=ch-ch=ch, -n=ch-n=ch, -n=ch-ch=n-, -n=n-ch=ch, -n=ch-ch=ch, -n=ch-n=ch, -n=ch-ch=n-, -n=n-ch=ch-; r1 é hidrogênio; arila; formila; c1-c6 alquila opcionalmente substituída; c1-c6 alquilóxicarbonila; r2 é oh; halo; c2-c6 alquinila opcionalmente substituída; carbonila substituída; carboxila; cn; nitro; amino; amino substituído; polihalometila; polihlometiltio; -s(=o)rr6; c(=nh)r6; r2a é cn;amino; amino substituído; c1-c6 alquila opcionalmente substituída; halo; c1-6 alquilóxi opcionalmente substituído carbonila substituída; -ch=n-nh-c(=o)-r16; c1-6 alquilóxi c1-6 alquila opcionalmente substituída; c2-6 alquenila ou c2-6 alquinila opcionalmente substituída; -c(=n-o-r8)-c1-4 alquila; r7 ou -x3-r7; x1 é -nr1 -, -o-, -c(=))-, ch2, -choh-, s-, -s(=o)-; r3 é cn; amino; c1-c6 alquila; halo; c1-c6 alquilóxi opcionalmente substituido; carbonila substituída; -ch=n-nh-c(=o)-r16; c1-c6 alquila substituída;c2-c6 alquenila ou c2-c6 alquinila opcionalmente substituída; -c(=n-o-r8)-c1-4 alquila; r7; -x3-r7; r4 é halo; oh; c1-6 alquila opcionalmente substituída; c2-6 alquenila ou c2-6 alquinila; c3-7 cicloalquila; c1-6 alquilóxi; cn; nitro; polihalo c1-6 alquila; polihalo c1-6 alquilóxi; carbonila substituída; formila; amino; mono- ou di(c1-4 alquil)amino ou r7; r5 é -y-cqh2q-l ou cqh2q-y-c2h2r-l; l é arila ou het; processos para o preparo desses compostos, composições farmacêuticas compreendendo esses compostos como ingredientes ativo e o uso desses compostos para a prevenção ou tratamento de infecção pelo hiv.
BRPI0515935A 2004-09-30 2005-09-29 pirimidinas heterociclil- ou 5-carbo substituídas para inibição de hiv, e composição farmacêutica BRPI0515935B8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP04104814 2004-09-30
PCT/EP2005/054931 WO2006035068A2 (en) 2004-09-30 2005-09-29 Hiv inhibiting 5-carbo- or heterocyclic substituted pyrimidines

Publications (3)

Publication Number Publication Date
BRPI0515935A BRPI0515935A (pt) 2008-08-12
BRPI0515935B1 BRPI0515935B1 (pt) 2019-11-19
BRPI0515935B8 true BRPI0515935B8 (pt) 2021-05-25

Family

ID=34929640

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0515935A BRPI0515935B8 (pt) 2004-09-30 2005-09-29 pirimidinas heterociclil- ou 5-carbo substituídas para inibição de hiv, e composição farmacêutica

Country Status (17)

Country Link
US (1) US7531548B2 (pt)
EP (1) EP1797048B1 (pt)
JP (1) JP5162245B2 (pt)
KR (1) KR20070057798A (pt)
CN (1) CN101031550B (pt)
AR (1) AR050970A1 (pt)
AT (1) ATE520672T1 (pt)
AU (1) AU2005288865B2 (pt)
BR (1) BRPI0515935B8 (pt)
CA (1) CA2573976C (pt)
ES (1) ES2371924T3 (pt)
IL (1) IL180760A (pt)
MX (1) MX2007003798A (pt)
RU (1) RU2403244C2 (pt)
TW (1) TW200626560A (pt)
WO (1) WO2006035068A2 (pt)
ZA (1) ZA200702655B (pt)

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ES2651349T3 (es) 2005-06-08 2018-01-25 Rigel Pharmaceuticals, Inc. Composiciones y métodos para la inhibición de la ruta JAK
AU2007233737B2 (en) * 2006-03-30 2012-11-29 Janssen Sciences Ireland Uc HIV inhibiting 5-amido substituted pyrimidines
DE602007009508D1 (de) * 2006-03-30 2010-11-11 Little Island Co Cork Hiv-inhibierende 5-(hydroxymethylen- und aminomethylen) substituierte pyrimidine
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Also Published As

Publication number Publication date
JP5162245B2 (ja) 2013-03-13
IL180760A (en) 2013-02-28
TW200626560A (en) 2006-08-01
JP2008514680A (ja) 2008-05-08
CA2573976C (en) 2014-04-29
RU2007116161A (ru) 2008-11-10
ATE520672T1 (de) 2011-09-15
WO2006035068A3 (en) 2006-08-31
AU2005288865B2 (en) 2012-07-19
US7531548B2 (en) 2009-05-12
EP1797048A2 (en) 2007-06-20
CN101031550B (zh) 2015-05-27
CA2573976A1 (en) 2006-04-06
BRPI0515935B1 (pt) 2019-11-19
MX2007003798A (es) 2007-04-23
AR050970A1 (es) 2006-12-06
AU2005288865A1 (en) 2006-04-06
CN101031550A (zh) 2007-09-05
IL180760A0 (en) 2007-06-03
ES2371924T3 (es) 2012-01-11
US20070208022A1 (en) 2007-09-06
ZA200702655B (en) 2008-09-25
BRPI0515935A (pt) 2008-08-12
KR20070057798A (ko) 2007-06-07
RU2403244C2 (ru) 2010-11-10
EP1797048B1 (en) 2011-08-17
WO2006035068A2 (en) 2006-04-06

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B25A Requested transfer of rights approved

Owner name: JANSSEN SCIENCES IRELAND UC (IE)

B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
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